高等学校化学学报2025，Vol.46Issue(5)：54-62,9.DOI:10.7503/cjcu20240548
含硫肽结构的噻肟酰胺衍生物的设计、合成与抗菌活性
Design,Synthesis and Antibacterial Activities of Thioxime Amide Derivatives Containing Thiopeptide
摘要
Abstract
In order to obtain novel antibacterial compounds,using the principle of pharmacophore assembly,twenty-four novel thioxime amide derivatives containing thiopeptide were designed and synthesized by combining active fragments of amino thiazole,oxime and thiopeptides,and confirmed by means of nuclear magnetic resonance hydrogen spectroscopy(1H NMR),nuclear magnetic resonance carbon spectroscopy(13C NMR)and elemental analysis.The antibacterial activities test results showed that these derivatives have significant activity against Gram positive bacteria.the minimum inhibitory concentration(MIC)values of compound 5u against S.aureus and methicillin-resistant S.aureus(MRSA)were 0.25 µg/mL and 2 µg/mL respectively,the MIC values of 5v against S.aureus and MRSA were 0.5 µg/mL and 2 µg/mL,respectively.Its anti-S.aureus activity was superior to that of the control drug oxacillin(MIC=0.5 µg/mL)or relatively,and its anti-MRSA activity was significantly better than that of the control drug(MIC＞128 µg/mL),which will be further developed as novel candidates for antibacterial drugs.关键词
硫肽/噻肟酰胺衍生物/药物设计/合成/抗菌活性Key words
Thiopeptide/Thioxime amide derivative/Drug design/Synthesis/Antibacterial activity分类
化学引用本文复制引用
佘慧娴,陈阳密,杨家强..含硫肽结构的噻肟酰胺衍生物的设计、合成与抗菌活性[J].高等学校化学学报,2025,46(5):54-62,9.基金项目
贵州省科技计划项目(批准号:黔科合基础-ZK[2024]一般265)和国家级大学生创新创业训练计划项目(批准号:202310661006)资助. Supported by the Guizhou Provincial Science and Technology Plan Project of China(No.Qiankehe Foundation ZK[2024]265)and the National College Students'Innovation and Entrepreneurship Training Program,China(No.202310661006). （批准号:黔科合基础-ZK[2024]一般265）
